Synthesis and evaluation of 5′-modified 2′-deoxyadenosine analogues as anti-hepatitis C virus agents

Synthesis and evaluation of 5′-modified 2′-deoxyadenosine analogues as anti-hepatitis C virus agents
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DOI:
10.1016/j.bmcl.2008.07.015
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发表时间:
2008-08-15
影响因子:
2.7
通讯作者:
Maruyama, Tokumi
Maruyama, Tokumi
中科院分区:
医学4区
文献类型:
--
作者:
Ikejiri, Masahiro;Ohshima, Takayuki;Maruyama, Tokumi

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为了研究2 '-脱氧核苷的5'-修饰对其抗HCV活性的影响,合成了几种类似物并进行了评价。在这些类似物中,5 ′-脱氧-5 ′-苯酰化类似物表现出良好的抗HCV活性,EC(50)为15.1 μ M。预期该化合物通过不涉及通常已知的5 '-O-三磷酸化过程的一类机制起作用。(C)2008爱思唯尔有限公司版权所有。
In order to study the effect of 5'-modification of 2'-deoxynucleoside on its anti-HCV activity, several analogues were synthesized and evaluated. Among the analogues, a 5'-deoxy-5'-phenacylated analogue exhibited a good anti-HCV activity with an EC(50) of 15.1 mu M. This compound is expected to operate via a type of mechanism that does not involve a generally known 5'-O-triphosphorylation process. (C) 2008 Elsevier Ltd. All rights reserved.